In vitro and computational investigations of novel synthetic carboxamide-linked pyridopyrrolopyrimidines with potent activity as SARS-CoV-2-M Pro inhibitors

A Aljuhani, HEA Ahmed, SK Ihmaid, AM Omar… - RSC …, 2022 - pubs.rsc.org
An essential target for COVID-19 is the main protease of SARS-CoV-2 (Mpro). With the
objective of targeting this receptor, a novel set of pyrido [1, 2-a] pyrrolo [2, 3-d] pyrimidines …

A review on multipurpose potential of bioactive heterocycle quinoxaline

G Chawla, O Gupta, T Pradhan - ChemistrySelect, 2023 - Wiley Online Library
In last few decades, nitrogen‐containing heterocycles have maintained their status as an
important core of FDA‐approved drugs and medicinally active compounds. Quinoxaline is …

Robust antiviral activity of commonly prescribed antidepressants against emerging coronaviruses: in vitro and in silico drug repurposing studies

O Kutkat, Y Moatasim, AA Al‐Karmalawy… - Scientific Reports, 2022 - nature.com
During the current coronavirus disease 2019 (COVID-19) pandemic, symptoms of
depression are commonly documented among both symptomatic and asymptomatic …

Apoptosis induction, PARP-1 inhibition, and cell cycle analysis of leukemia cancer cells treated with novel synthetic 1, 2, 3-triazole-chalcone conjugates

EM Othman, EA Fayed, EM Husseiny, HS Abulkhair - Bioorganic Chemistry, 2022 - Elsevier
Leukemia is a life-threatening nonepithelial malignant disorder that is characterized by
uncontrolled growth of the hematopoietic cells. To date, there are still unmet needs for …

From triazolophthalazines to triazoloquinazolines: A bioisosterism-guided approach toward the identification of novel PCAF inhibitors with potential anticancer activity

MH El-Shershaby, A Ghiaty, AH Bayoumi… - Bioorganic & Medicinal …, 2021 - Elsevier
Inhibition of PCAF bromodomain has been validated as a promising strategy for the
treatment of cancer. In this study, we report the bioisosteric modification of the first reported …

The antimicrobial potential and pharmacokinetic profiles of novel quinoline-based scaffolds: synthesis and in silico mechanistic studies as dual DNA gyrase and …

MH El-Shershaby, KM El-Gamal, AH Bayoumi… - New Journal of …, 2021 - pubs.rsc.org
The resistance of pathogenic microbes to currently available antimicrobial agents has been
considered a global alarming concern. Hence, close attention should be paid to the …

Pharmacophore‐linked pyrazolo[3,4‐d]pyrimidines as EGFR‐TK inhibitors: Synthesis, anticancer evaluation, pharmacokinetics, and in silico mechanistic studies

AA Gaber, AM El‐Morsy, FF Sherbiny… - Archiv Der …, 2021 - Wiley Online Library
Targeting the epidermal growth factor receptors (EGFRs) with small inhibitor molecules has
been validated as a potential therapeutic strategy in cancer therapy. Pyrazolo [3, 4‐d] …

[HTML][HTML] An insight into the therapeutic impact of quinoxaline derivatives: Recent advances in biological activities (2020–2024)

AM Waseem, RM Elmagzoub, MMM Abdelgadir… - Results in …, 2024 - Elsevier
Quinoxaline derivatives have garnered significant attention due to their wide-ranging
therapeutic applications. Research from 2020 to 2024 has demonstrated their potent …

The anticancer and EGFR-TK/CDK-9 dual inhibitory potentials of new synthetic pyranopyrazole and pyrazolone derivatives: X-ray crystallography, in vitro, and in silico …

A Musa, SK Ihmaid, DL Hughes, MA Said… - Journal of …, 2023 - Taylor & Francis
Abstract Treatment options for the management of breast cancer are still inadequate. This
inadequacy is attributed to the lack of effective targeted medications, often resulting in the …

Rationale design, synthesis, cytotoxicity evaluation, and in silico mechanistic studies of novel 1, 2, 3-triazoles with potential anticancer activity

EM Othman, EA Fayed, EM Husseiny… - New Journal of …, 2022 - pubs.rsc.org
A new set of 1, 2, 3-triazoles was designed and synthesized to evaluate their potential to
inhibit the growth of cancer cells. Thiazole, thiazolone, and hydrazine as effective fragments …